Naringenin-Loaded TPGS Polymeric Nanosuspension: In-Vitro and In-Vivo Anti-Inflammatory Activity
Naringenin, (NAR) from Citrus grandis(L.) Osbeck, family Rutaceae, exhibit extensive pharmacological action, lacks significance in application due to low aqueous solubility approximately 0.214 mg/ml, which results in low bioavailability of 5.8%. Nanosuspension of NAR (NARNS) was prepared in our previous studies using high pressure homogenization adding various polymers. All these formulations were characterized and as a continuation of our work formulations was further evaluated for their anti-inflammatory activity by in-vitro and in-vivo methods. Denaturation of protein method and membrane stabilization methods were chosen for in-vitro evaluation. In-vivo studies performed were acute inflammatory studies (carrageenan-induced paw oedema) and chronic inflammatory studies (cotton pellet granuloma) on Wistar albino rats. The studies demonstrated that the NAR and NARNS at a dose of 50 mg/kg P.O. have a potent activity compared to the standard drug diclofenac. The percentage protection against inflammation exhibited by NARNS was highly significant compared to NAR.
Alhakmani F., 2013. Estimation of total phenolic content, in-vitro antioxidant and anti-inflammatory activity of flowers of Moringaoleifera. Asian. Pac. J. Trop. Biomed. 3:623-627.
Ameer B., 1996. Flavanone absorption after naringin, hesperidin, and citrus administration. Clin.Pharmacol.Ther. 60:34-40.
Antonisamy P., Agastian P., Kang C.W., Kim N.S., Kim J.H., 2017. Anti-inflammatory activity of rhein isolated from the flowers of Cassia fistula L. and possible underlying mechanisms. Saudi journal of biological sciences. 28.
Cavia-Saiz M., 2010. Antioxidant properties, radical scavenging activity and biomolecule protection capacity of flavonoid NAR and its glycoside naringin: a comparative study. J. Sci. Food. Agri. 90:1238-1244.
Chathurdevi G., Umagowrie S., 2017. Potent bioactive metabolites of casuarinajunghuhnianamiq. Roots–a therapeutic approach. Int. J. Pharm. Sci.9:158-165.
Choi J.S., 1991. Antihyperlipidemic effect of flavonoids from Prunusdavidiana. J. Nat. Prod. 54: 218-224.
Dou w., 2009. Protective effect on NAR against experimental colitis via suppression of Toll-like receptor 4/ NF- kB signaling. Br.J.Nutr. 110(4):599- 608.
Elias G., 1988. Inhibition of albumin denaturation and anti-inflammatory activity of dehydrozingerone and its analogs. Indian. J. Exp. Biol. 26: 540-542.
Elisha I. L, Dzoyem J. P., McGaw L. J., Botha F. S., Eloff J. N. 2016. The anti-arthritic, anti-inflammatory, antioxidant activity and relationships with total phenolics and total flavonoids of nine South African plants used traditionally to treat arthritis. BMC complementary and alternative medicine. 16:307.
Fatma Alhakmani., 2014.Determination of total phenolic,in-vitro antioxidant and anti-inflammatory activity of seeds and fruits of Zizyphusspina –Christi grown in Oman. Asian.Pac. J. Trop. Biomed. 4: 656–660.
Ferrero-Miliani L., 2007. Chronic inflammation: importance of NOD2 and NALP3 in interleukin-1beta generation. Clin. Exp. Immunol., 2: 147.
Gambhire M., 2008. Evaluation of anti-inflammatory activity of methanol extract of BarleriaCristata leaves by in-vivo and in-vitro methods. The Internet J.Pharmacol. 7:21-27.
Gandhidasan R., 1991. Anti-inflamattory action of Laneacoromondelica by HRBC membranestabilisation. Fitotherapia. 62:82-83.
Jain A.K., 2011. The effect of the oral administration of polymeric nanoparticles on the efficacy and toxicity of tamoxifen. Biomaterials. 32:503–515.
James O., 2009. In-vitro and in-vivo studies on the anti-oxidative activities, membrane stabilization and cytotoxicity of water spinach from ipogi ponds (Nigeria).Int. J.Pharmtech. Research. 1:474-482.
Jayaraman J., 2012. Anti-inflammatory role of naringenin in rats with ethanol induced liver injury. ToxicolMech Methods. 22:568-576.
Leelaprakash G., Dass S.M. 2011. In vitro anti-inflammatory activity of methanol extract of Enicostemmaaxillare. International Journal of Drug Development and Research. 3(3):189-96.
Mizushima Y., Kobayashi M., 1968. Interaction of anti-inflammatory drugs with serum proteins, especially with some biologically active proteins. J Pharm Pharmacol. 20:169- 73.
Mundekkad Deepa., Menon B., Darsanb., Chidambaram Ramalingam. 2015. In vitro Evaluation Of The Antioxidant, Anti-Inflammatory And Antiproliferative Activities Of The Leaf Extracts Of Excoecaria AgallochaL .Int. J. Pharm Sci. 7:346-352.
Nsonde Ntandou G.F., 2010. Analgesic and anti -inflammatory effects of Cassia siamea Lam. Stem bark extracts. J. Ethnopharmacol. 127:108-111.
Panthong A., 2003. Anti-inflammatory and antipyretic properties of Clerodendrum petasites S. Moore. J.Ethnopharmacol. 85:151–156.
Rao A.B., Sisodia P., Sattur P.B. 1989. Lysosomal membrane stabilization by antiinflammatory drugs. Indian journal of experimental biology. 27:1097-8.
Singh M., Kumar V., Singh I., Gauttam V., Kalia A. N., 2010. Anti-inflammatory activity of aqueous extract of Mirabilis jalapa Linn. leaves. Pharmacognosy research. 2(6):364.
Sumathi R., 2017. Formulation and evaluation of polymeric nanosuspension of NAR. Int. J. App. Pharm. 9:60-70.
Sumana Sarkhel., 2016. Evaluation of the anti-inflammatory activities of Quillajasaponaria Mol. saponin extracts in mice.Toxicol.reports. 3:1-3.
Swingle K.F., 1972. Phases of the inflammatory response to subcutaneous implantation of a cotton pellet and their modification by certain anti-inflammatory agents. J.Pharmacol.Exp.Ther. 183:226–234.
Varadarasu M., 2007. Evaluation of anti-inflammatory and membrane stabilizing properties of ethanol extract of Cansjerarheedii J. Gmelin (Opiliaceae). Iranian Journal of Pharmacology and Therapeutics. 235-237.
Wen J., 2010. Preparation and physiochemical properties of the complex of NAR with hydroxypropyl-cyclodextrin. Molecules. 15:4401–4407.
William L.S.,1989. The eicosanoids and their biochemical mechanism of action. Biochem J. 259:315-324.
Winter C.A., Risley and G.W., 1962. Nuss.Carrageenan-induced oedema in the hind paw of rat as an assay for anti-inflammatory activity.Proc. Soc. Exp. Biol.Ther. 111:544-547.
Wolfe M.M., David R.L.,1999. Lichtenstein: Gastrointestinal toxicity of Non-steroidal anti-inflammatory drugs. N Engl J Med. 340:1888-1899.
Yen F.L., 2008. NAR-loaded nanoparticles improve the physicochemical properties and the hepatoprotective effect of NAR in orally administrated rats with CCl4-induced acute liver failure. Pharm Res. 26:893–902.
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